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Identification
NameLiothyronine
Accession NumberDB00279  (APRD01074)
TypeSmall Molecule
GroupsApproved, Vet Approved
Description

The L-triiodothyronine (T3, liothyronine) thyroid hormone is normally synthesized and secreted by the thyroid gland in much smaller quantities than L-tetraiodothyronine (T4, levothyroxine, L-thyroxine). Most T3 is derived from peripheral monodeiodination of T4 at the 5 position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3. [PubChem]

Structure
Thumb
Synonyms
3,3',5-triiodo-L-thyronine
3,5,3'-Triiodo-L-thyronine
3,5,3'-Triiodothyronine
3,5,3'TRIIODOTHYRONINE
4-(4-Hydroxy-3-iodophenoxy)-3,5-diiodo-L-phenylalanine
L-3,5,3'-Triiodothyronine
L-T3
Liothyronine
Liothyroninum
Liotironina
O-(4-hydroxy-3-iodophenyl)-3,5-diiodo-L-tyrosine
T3
Tertroxin
Tresitope
Triiodothyronine
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cytomeltablet25 ug/1oralPfizer Laboratories Div Pfizer Inc1956-05-08Not applicableUs
Cytomeltablet5 ug/1oralPfizer Laboratories Div Pfizer Inc1956-05-08Not applicableUs
Cytomeltablet5 ug/1oralPhysicians Total Care, Inc.2004-05-03Not applicableUs
Cytomeltablet25 ug/1oralPhysicians Total Care, Inc.2002-12-30Not applicableUs
Cytomeltablet5 mcgoralPfizer Canada Inc1993-12-31Not applicableCanada
Cytomeltablet5 ug/1oralA S Medication Solutions Llc1956-05-08Not applicableUs
Cytomeltablet25 mcgoralPfizer Canada Inc1993-12-31Not applicableCanada
Cytomeltablet25 ug/1oralA S Medication Solutions Llc1956-05-08Not applicableUs
Cytomeltablet50 ug/1oralPfizer Laboratories Div Pfizer Inc1956-05-08Not applicableUs
Triostatinjection10 ug/mLintravenousJHP Pharmaceuticals LLC2007-10-01Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Liothyronine Sodiumtablet50 ug/1oralSigmapharm Laboratories, LLC2012-11-30Not applicableUs
Liothyronine Sodiumtablet25 ug/1oralKAISER FOUNDATION HOSPITALS2009-08-29Not applicableUs
Liothyronine Sodiumtablet25 ug/1oralPd Rx Pharmaceuticals, Inc.2009-03-23Not applicableUs
Liothyronine Sodiumtablet25 ug/1oralPaddock Laboratories, Inc.2009-03-23Not applicableUs
Liothyronine Sodiumtablet25 ug/1oralGolden State Medical Supply, Inc.2014-08-28Not applicableUs
Liothyronine Sodiumtablet25 ug/1oralSigmapharm Laboratories, LLC2012-11-30Not applicableUs
Liothyronine Sodiumtablet5 ug/1oralGolden State Medical Supply, Inc.2014-08-28Not applicableUs
Liothyronine Sodiumtablet5 ug/1oralPaddock Laboratories, Inc.2009-03-23Not applicableUs
Liothyronine Sodiumtablet5 ug/1oralSigmapharm Laboratories, LLC2012-11-30Not applicableUs
Liothyronine Sodiumtablet25 ug/1oralLake Erie Medical DBA Quality Care Products LLC2012-11-30Not applicableUs
Liothyronine Sodiumtablet50 ug/1oralMylan Pharmaceuticals Inc.2013-01-23Not applicableUs
Liothyronine Sodiuminjection, solution10 ug/mLintravenousX Gen Pharmaceuticals, Inc.2005-08-17Not applicableUs
Liothyronine Sodiumtablet25 ug/1oralNorthwind Pharmaceuticals, LLC2014-11-12Not applicableUs
Liothyronine Sodiumtablet25 ug/1oralMylan Pharmaceuticals Inc.2013-01-23Not applicableUs
Liothyronine Sodiumtablet25 ug/1oralCarilion Materials Management2009-03-23Not applicableUs
Liothyronine Sodiumtablet5 ug/1oralAidarex Pharmaceuticals LLC2009-03-23Not applicableUs
Liothyronine Sodiumtablet50 ug/1oralNorthwind Pharmaceuticals2014-12-29Not applicableUs
Liothyronine Sodiumtablet5 ug/1oralMylan Pharmaceuticals Inc.2013-01-23Not applicableUs
Liothyronine Sodiumtablet50 1/1oralStat Rx USA2009-03-20Not applicableUs
Liothyronine Sodiumtablet5 ug/1oralCarilion Materials Management2009-03-23Not applicableUs
Liothyronine Sodiumtablet50 ug/1oralPd Rx Pharmaceuticals, Inc.2009-03-23Not applicableUs
Liothyronine Sodiumtablet5 ug/1oralKAISER FOUNDATION HOSPITALS2009-08-28Not applicableUs
Liothyronine Sodiumtablet25 ug/1oralMedsource Pharmaceuticals2009-03-23Not applicableUs
Liothyronine Sodiumtablet50 ug/1oralPaddock Laboratories, Inc.2009-03-23Not applicableUs
Liothyronine Sodiumtablet50 ug/1oralGolden State Medical Supply, Inc.2014-08-28Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
TertroxinAspen Pharmacare
Brand mixtures
NameLabellerIngredients
Np Thyroid 30Acella Pharmaceuticals, LLC
Np Thyroid 60Acella Pharmaceuticals, LLC
Np Thyroid 90Acella Pharmaceuticals, LLC
Salts
Name/CASStructureProperties
Liothyronine Sodium
55-06-1
Thumb
  • InChI Key: SBXXSUDPJJJJLC-YDALLXLXSA-M
  • Monoisotopic Mass: 672.77198278
  • Average Mass: 672.9553
DBSALT000321
Categories
UNII06LU7C9H1V
CAS number6893-02-3
WeightAverage: 650.9735
Monoisotopic: 650.790038137
Chemical FormulaC15H12I3NO4
InChI KeyInChIKey=AUYYCJSJGJYCDS-LBPRGKRZSA-N
InChI
InChI=1S/C15H12I3NO4/c16-9-6-8(1-2-13(9)20)23-14-10(17)3-7(4-11(14)18)5-12(19)15(21)22/h1-4,6,12,20H,5,19H2,(H,21,22)/t12-/m0/s1
IUPAC Name
(2S)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-diiodophenyl]propanoic acid
SMILES
N[C@@H](CC1=CC(I)=C(OC2=CC(I)=C(O)C=C2)C(I)=C1)C(O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as diphenylethers. These are aromatic compounds containing two benzene rings linked to each other through an ether group.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassDiphenylethers
Direct ParentDiphenylethers
Alternative Parents
Substituents
  • Diphenylether
  • 3-phenylpropanoic-acid
  • Diaryl ether
  • L-alpha-amino acid
  • Amphetamine or derivatives
  • Alpha-amino acid or derivatives
  • Alpha-amino acid
  • 2-iodophenol
  • 2-halophenol
  • Aralkylamine
  • Phenol
  • Iodobenzene
  • Halobenzene
  • Amino fatty acid
  • Fatty acyl
  • Aryl iodide
  • Aryl halide
  • Monocarboxylic acid or derivatives
  • Ether
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Organoiodide
  • Organohalogen compound
  • Primary aliphatic amine
  • Carbonyl group
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationUsed as replacement or supplemental therapy in patients with hypothyroidism of any etiology, except transient hypothyrodism during the recovery phase of subacute thyroiditis.
PharmacodynamicsThyroid hormone drugs are natural or synthetic preparations containing T4 or T3 or both. T4 and T3 are produced in the human thyroid gland by the iodination and coupling of the amino acid tyrosine. Liothyronine (T3) contains three atoms of iodine and is formed by the coupling of one molecule of diiodotyrosine (DIT) with one molecule of monoiodotyrosine (MIT). These hormones enhance oxygen consumption by most tissues of the body and increase the basal metabolic rate and the metabolism of carbohydrates, lipids and proteins. Thus, they exert a profound influence on every organ system in the body and are of particular importance in the development of the central nervous system.
Mechanism of actionThe hormones, T4 and T3, are tyrosine-based hormones produced by the thyroid gland. Iodine is an important component in their synthesis. The major form of thyroid hormone in the blood is thyroxine (T4). This is converted to the more active liothyronine form by deiodinases in peripheral tissues. Liothyronine acts on the body to increase the basal metabolic rate, affect protein synthesis and increase the body's sensitivity to catecholamines (such as adrenaline). The thyroid hormones are essential to proper development and differentiation of all cells of the human body. To various extents T4 and T3 regulate protein, fat and carbohydrate metabolism. Their most pronounced effect is on how human cells use energetic compounds. The thyroid hormone derivatives bind to the thyroid hormone receptors initially to initiate their downstream effects.
Related Articles
Absorption95% in 4 hours
Volume of distributionNot Available
Protein binding99.7%
Metabolism
SubstrateEnzymesProduct
Liothyronine
Not Available
Triiodothyronine sulfateDetails
Route of eliminationNot Available
Half life2.5 days
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Thyroid hormone synthesisMetabolicSMP00716
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.7212
Blood Brain Barrier-0.6886
Caco-2 permeable-0.653
P-glycoprotein substrateNon-substrate0.5321
P-glycoprotein inhibitor INon-inhibitor0.9175
P-glycoprotein inhibitor IINon-inhibitor0.9709
Renal organic cation transporterNon-inhibitor0.8891
CYP450 2C9 substrateNon-substrate0.8309
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6847
CYP450 1A2 substrateNon-inhibitor0.5924
CYP450 2C9 inhibitorNon-inhibitor0.7037
CYP450 2D6 inhibitorNon-inhibitor0.923
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.831
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8459
Ames testNon AMES toxic0.7591
CarcinogenicityNon-carcinogens0.9148
BiodegradationNot ready biodegradable0.9693
Rat acute toxicity2.7082 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9697
hERG inhibition (predictor II)Non-inhibitor0.8508
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • X gen pharmaceuticals inc
  • Jhp pharmaceuticals llc
  • King pharmaceuticals inc
  • Coastal pharmaceuticals inc
  • Mylan pharmaceuticals inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral25 mcg
Tabletoral5 mcg
Injection, solutionintravenous10 ug/mL
Tabletoral25 ug/1
Tabletoral5 ug/1
Tabletoral50 1/1
Tabletoral50 ug/1
Tablettopical
Tabletoral
Injectionintravenous10 ug/mL
Prices
Unit descriptionCostUnit
Triostat 10 mcg/ml vial627.9USD ml
Cytomel 50 mcg tablet1.89USD tablet
Liothyronine Sodium 50 mcg tablet1.69USD tablet
Liothyronine sod 50 mcg tablet1.62USD tablet
Cytomel 25 mcg tablet1.21USD tablet
Cytomel 25 mcg Tablet1.2USD tablet
Cytomel 5 mcg Tablet1.11USD tablet
Liothyronine Sodium 25 mcg tablet1.09USD tablet
Liothyronine sod 25 mcg tablet1.06USD tablet
Cytomel 5 mcg tablet0.89USD tablet
Liothyronine Sodium 5 mcg tablet0.84USD tablet
Liothyronine sod 5 mcg tablet0.81USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point236-237U.S. Patent 2,823,164.
water solubility3.96 mg/L (at 37 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.9Not Available
logS-5.22ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.0195 mg/mLALOGPS
logP0.82ALOGPS
logP2.8ChemAxon
logS-4.5ALOGPS
pKa (Strongest Acidic)0.3ChemAxon
pKa (Strongest Basic)9.48ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area92.78 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity113.43 m3·mol-1ChemAxon
Polarizability43.92 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 10V, N/A (Annotated)splash10-000i-0009001000-1d47041336da63b556e4View in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 25V, N/A (Annotated)splash10-000i-1009001000-15f70073b9018f013c9cView in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 40V, N/A (Annotated)splash10-000i-0009000000-71c231d7a3ab505815ffView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, Negativesplash10-0udi-0000009000-f932659d1e6d8a622985View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, Negativesplash10-0udi-0000009000-6506a7a71dab928abfb0View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, Negativesplash10-0fc0-0700119000-1df6db0e3031eb2739faView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, Negativesplash10-004i-0900000000-973fc871534b19242cc8View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, Negativesplash10-004i-0900000000-ac3c4a198bb017dc7cccView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, Positivesplash10-0udi-0000009000-2770ece749a9fa1042f4View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, Positivesplash10-0udi-0000009000-881174c66da97022d645View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, Positivesplash10-0a4i-0000019000-6f798ae76702a3053339View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, Positivesplash10-0a4i-0000219000-d2ca9f0cc3c1b47176b5View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, Positivesplash10-056r-0021915000-6f3810619f383bce651aView in MoNA
1D NMR1H NMR SpectrumNot Available
2D NMR[1H,13C] 2D NMR SpectrumNot Available
References
Synthesis Reference

Martin Beasley, David Hause, Irwin Klein, Charles Pamplin, David Reynolds, Kevin Sills, “Controlled release pharmaceutical compositions of liothyronine and methods of making and using the same.” U.S. Patent US20060246133, issued November 02, 2006.

US20060246133
General References
  1. Uchino H, Kanai Y, Kim DK, Wempe MF, Chairoungdua A, Morimoto E, Anders MW, Endou H: Transport of amino acid-related compounds mediated by L-type amino acid transporter 1 (LAT1): insights into the mechanisms of substrate recognition. Mol Pharmacol. 2002 Apr;61(4):729-37. [PubMed:11901210 ]
External Links
ATC CodesH03AA03H03AA02
AHFS Codes
  • 68:36.04
PDB EntriesNot Available
FDA labelDownload (40.8 KB)
MSDSDownload (73.4 KB)
Interactions
Drug Interactions
Drug
AcenocoumarolLiothyronine may increase the anticoagulant activities of Acenocoumarol.
AminophyllineThe metabolism of Aminophylline can be increased when combined with Liothyronine.
AmitriptylineLiothyronine may increase the arrhythmogenic activities of Amitriptyline.
AmoxapineLiothyronine may increase the arrhythmogenic activities of Amoxapine.
Calcium AcetateThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Calcium Acetate.
Calcium carbonateThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Calcium carbonate.
Calcium ChlorideThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Calcium Chloride.
Calcium citrateThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Calcium citrate.
Calcium gluconateThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Calcium gluconate.
CarbamazepineThe serum concentration of Liothyronine can be decreased when it is combined with Carbamazepine.
ChlorotrianiseneThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Chlorotrianisene.
CholestyramineThe serum concentration of Liothyronine can be decreased when it is combined with Cholestyramine.
CiprofloxacinThe serum concentration of Liothyronine can be decreased when it is combined with Ciprofloxacin.
CitalopramThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Citalopram.
ClomipramineLiothyronine may increase the arrhythmogenic activities of Clomipramine.
ColesevelamThe serum concentration of Liothyronine can be decreased when it is combined with Colesevelam.
ColestipolThe serum concentration of Liothyronine can be decreased when it is combined with Colestipol.
DesipramineLiothyronine may increase the arrhythmogenic activities of Desipramine.
DesogestrelThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Desogestrel.
DicoumarolLiothyronine may increase the anticoagulant activities of Dicoumarol.
DoxepinLiothyronine may increase the arrhythmogenic activities of Doxepin.
DrospirenoneThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Drospirenone.
EscitalopramThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Escitalopram.
EstradiolThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Estradiol.
Estrone sulfateThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Estropipate.
Ethinyl EstradiolThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Ethinyl Estradiol.
Ethynodiol diacetateThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Ethynodiol.
FluoxetineThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Fluoxetine.
FluvoxamineThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Fluvoxamine.
FosphenytoinThe serum concentration of Liothyronine can be decreased when it is combined with Fosphenytoin.
ImipramineLiothyronine may increase the arrhythmogenic activities of Imipramine.
Lanthanum carbonateThe serum concentration of Liothyronine can be decreased when it is combined with Lanthanum carbonate.
MestranolThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Mestranol.
NorethisteroneThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Norethindrone.
NorgestimateThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Norgestimate.
NortriptylineLiothyronine may increase the arrhythmogenic activities of Nortriptyline.
ParoxetineThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Paroxetine.
PhenytoinThe serum concentration of Liothyronine can be decreased when it is combined with Phenytoin.
PiracetamThe risk or severity of adverse effects can be increased when Piracetam is combined with Liothyronine.
Polystyrene sulfonateThe serum concentration of Liothyronine can be decreased when it is combined with Polystyrene sulfonate.
ProtriptylineLiothyronine may increase the arrhythmogenic activities of Protriptyline.
RifampicinThe serum concentration of Liothyronine can be decreased when it is combined with Rifampicin.
SertralineThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Sertraline.
Sodium Iodide I-131The therapeutic efficacy of Sodium Iodide I-131 can be decreased when used in combination with Liothyronine.
TheophyllineThe metabolism of Theophylline can be increased when combined with Liothyronine.
TrimipramineLiothyronine may increase the arrhythmogenic activities of Trimipramine.
VilazodoneThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Vilazodone.
VortioxetineThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Vortioxetine.
WarfarinLiothyronine may increase the anticoagulant activities of Warfarin.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Isoform Alpha-1: Nuclear hormone receptor that can act as a repressor or activator of transcription. High affinity receptor for thyroid hormones, including triiodothyronine and thyroxine.Isoform Alpha-2: Does not bind thyroid hormone and functions as a weak dominant negative inhibitor of thyroid hormone action.
Gene Name:
THRA
Uniprot ID:
P10827
Molecular Weight:
54815.055 Da
References
  1. Jiang W, Miyamoto T, Kakizawa T, Sakuma T, Nishio S, Takeda T, Suzuki S, Hashizume K: Expression of thyroid hormone receptor alpha in 3T3-L1 adipocytes; triiodothyronine increases the expression of lipogenic enzyme and triglyceride accumulation. J Endocrinol. 2004 Aug;182(2):295-302. [PubMed:15283690 ]
  2. Kariv R, Enden A, Zvibel I, Rosner G, Brill S, Shafritz DA, Halpern Z, Oren R: Triiodothyronine and interleukin-6 (IL-6) induce expression of HGF in an immortalized rat hepatic stellate cell line. Liver Int. 2003 Jun;23(3):187-93. [PubMed:12955882 ]
  3. Mai W, Janier MF, Allioli N, Quignodon L, Chuzel T, Flamant F, Samarut J: Thyroid hormone receptor alpha is a molecular switch of cardiac function between fetal and postnatal life. Proc Natl Acad Sci U S A. 2004 Jul 13;101(28):10332-7. Epub 2004 Jul 6. [PubMed:15240882 ]
  4. Sciaudone MP, Yao L, Schaller M, Zinn SA, Freake HC: Diethylenetriaminepentaacetic acid enhances thyroid hormone action by a transcriptional mechanism. Biol Trace Elem Res. 2004 Summer;99(1-3):219-31. [PubMed:15235154 ]
  5. Timmer DC, Bakker O, Wiersinga WM: Triiodothyronine affects the alternative splicing of thyroid hormone receptor alpha mRNA. J Endocrinol. 2003 Nov;179(2):217-25. [PubMed:14596673 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Nuclear hormone receptor that can act as a repressor or activator of transcription. High affinity receptor for thyroid hormones, including triiodothyronine and thyroxine.
Gene Name:
THRB
Uniprot ID:
P10828
Molecular Weight:
52787.16 Da
References
  1. Bernal J: Thyroid hormone receptors in brain development and function. Nat Clin Pract Endocrinol Metab. 2007 Mar;3(3):249-59. [PubMed:17315033 ]
  2. Gonzalez-Sancho JM, Garcia V, Bonilla F, Munoz A: Thyroid hormone receptors/THR genes in human cancer. Cancer Lett. 2003 Mar 31;192(2):121-32. [PubMed:12668276 ]
  3. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  4. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  5. Yen PM, Feng X, Flamant F, Chen Y, Walker RL, Weiss RE, Chassande O, Samarut J, Refetoff S, Meltzer PS: Effects of ligand and thyroid hormone receptor isoforms on hepatic gene expression profiles of thyroid hormone receptor knockout mice. EMBO Rep. 2003 Jun;4(6):581-7. [PubMed:12776178 ]
  6. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  7. Wu SY, Sadow PM, Refetoff S, Weiss RE: Tissue responses to thyroid hormone in a kindred with resistance to thyroid hormone harboring a commonly occurring mutation in the thyroid hormone receptor beta gene (P453T). J Lab Clin Med. 2005 Aug;146(2):85-94. [PubMed:16099238 ]
  8. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Identical protein binding
Specific Function:
Thyroid hormone-binding protein. Probably transports thyroxine from the bloodstream to the brain.
Gene Name:
TTR
Uniprot ID:
P02766
Molecular Weight:
15886.88 Da
References
  1. Eneqvist T, Lundberg E, Karlsson A, Huang S, Santos CR, Power DM, Sauer-Eriksson AE: High resolution crystal structures of piscine transthyretin reveal different binding modes for triiodothyronine and thyroxine. J Biol Chem. 2004 Jun 18;279(25):26411-6. Epub 2004 Apr 13. [PubMed:15082720 ]
  2. Palha JA: Transthyretin as a thyroid hormone carrier: function revisited. Clin Chem Lab Med. 2002 Dec;40(12):1292-300. [PubMed:12553433 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serine-type endopeptidase inhibitor activity
Specific Function:
Major thyroid hormone transport protein in serum.
Gene Name:
SERPINA7
Uniprot ID:
P05543
Molecular Weight:
46324.12 Da
References
  1. Palha JA: Transthyretin as a thyroid hormone carrier: function revisited. Clin Chem Lab Med. 2002 Dec;40(12):1292-300. [PubMed:12553433 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. Palha JA: Transthyretin as a thyroid hormone carrier: function revisited. Clin Chem Lab Med. 2002 Dec;40(12):1292-300. [PubMed:12553433 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibited by the grapefruit juice component naringin.
Gene Name:
SLCO1A2
Uniprot ID:
P46721
Molecular Weight:
74144.105 Da
References
  1. Fujiwara K, Adachi H, Nishio T, Unno M, Tokui T, Okabe M, Onogawa T, Suzuki T, Asano N, Tanemoto M, Seki M, Shiiba K, Suzuki M, Kondo Y, Nunoki K, Shimosegawa T, Iinuma K, Ito S, Matsuno S, Abe T: Identification of thyroid hormone transporters in humans: different molecules are involved in a tissue-specific manner. Endocrinology. 2001 May;142(5):2005-12. [PubMed:11316767 ]
  2. Friesema EC, Docter R, Moerings EP, Stieger B, Hagenbuch B, Meier PJ, Krenning EP, Hennemann G, Visser TJ: Identification of thyroid hormone transporters. Biochem Biophys Res Commun. 1999 Jan 19;254(2):497-501. [PubMed:9918867 ]
  3. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Abe T, Kakyo M, Tokui T, Nakagomi R, Nishio T, Nakai D, Nomura H, Unno M, Suzuki M, Naitoh T, Matsuno S, Yawo H: Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1. J Biol Chem. 1999 Jun 11;274(24):17159-63. [PubMed:10358072 ]
  2. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Molecular Weight:
77402.175 Da
References
  1. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893 ]
  2. Abe T, Unno M, Onogawa T, Tokui T, Kondo TN, Nakagomi R, Adachi H, Fujiwara K, Okabe M, Suzuki T, Nunoki K, Sato E, Kakyo M, Nishio T, Sugita J, Asano N, Tanemoto M, Seki M, Date F, Ono K, Kondo Y, Shiiba K, Suzuki M, Ohtani H, Shimosegawa T, Iinuma K, Nagura H, Ito S, Matsuno S: LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers. Gastroenterology. 2001 Jun;120(7):1689-99. [PubMed:11375950 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Organic anion transporter, capable of transporting pharmacological substances such as digoxin, ouabain, thyroxine, methotrexate and cAMP. May participate in the regulation of membrane transport of ouabain. Involved in the uptake of the dipeptidyl peptidase-4 inhibitor sitagliptin and hence may play a role in its transport into and out of renal proximal tubule cells. May be involved in the first...
Gene Name:
SLCO4C1
Uniprot ID:
Q6ZQN7
Molecular Weight:
78947.525 Da
References
  1. Mikkaichi T, Suzuki T, Onogawa T, Tanemoto M, Mizutamari H, Okada M, Chaki T, Masuda S, Tokui T, Eto N, Abe M, Satoh F, Unno M, Hishinuma T, Inui K, Ito S, Goto J, Abe T: Isolation and characterization of a digoxin transporter and its rat homologue expressed in the kidney. Proc Natl Acad Sci U S A. 2004 Mar 9;101(10):3569-74. Epub 2004 Mar 1. [PubMed:14993604 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Virus receptor activity
Specific Function:
The hepatic sodium/bile acid uptake system exhibits broad substrate specificity and transports various non-bile acid organic compounds as well. It is strictly dependent on the extracellular presence of sodium.(Microbial infection) Acts as a receptor for hepatitis B virus.
Gene Name:
SLC10A1
Uniprot ID:
Q14973
Molecular Weight:
38118.64 Da
References
  1. Friesema EC, Docter R, Moerings EP, Stieger B, Hagenbuch B, Meier PJ, Krenning EP, Hennemann G, Visser TJ: Identification of thyroid hormone transporters. Biochem Biophys Res Commun. 1999 Jan 19;254(2):497-501. [PubMed:9918867 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Thyroid hormone transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent high affinity transport of organic anions such as the thyroid hormones thyroxine (T4) and rT3. Other potential substrates, such as triiodothyronine (T3), 17-beta-glucuronosyl estradiol, estrone-3-sulfate and sulfobromophthalein (BSP) are transported with much lower efficiency. May play a signifiant role in regulating T4 flux into and out of the brain (By similarity).
Gene Name:
SLCO1C1
Uniprot ID:
Q9NYB5
Molecular Weight:
78695.625 Da
References
  1. Tohyama K, Kusuhara H, Sugiyama Y: Involvement of multispecific organic anion transporter, Oatp14 (Slc21a14), in the transport of thyroxine across the blood-brain barrier. Endocrinology. 2004 Sep;145(9):4384-91. Epub 2004 May 27. [PubMed:15166123 ]
  2. Pizzagalli F, Hagenbuch B, Stieger B, Klenk U, Folkers G, Meier PJ: Identification of a novel human organic anion transporting polypeptide as a high affinity thyroxine transporter. Mol Endocrinol. 2002 Oct;16(10):2283-96. [PubMed:12351693 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Thyroid hormone transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as the thyroid hormones T3 (triiodo-L-thyronine), T4 (thyroxine) and rT3, and of estrone-3-sulfate and taurocholate.
Gene Name:
SLCO4A1
Uniprot ID:
Q96BD0
Molecular Weight:
77192.505 Da
References
  1. Fujiwara K, Adachi H, Nishio T, Unno M, Tokui T, Okabe M, Onogawa T, Suzuki T, Asano N, Tanemoto M, Seki M, Shiiba K, Suzuki M, Kondo Y, Nunoki K, Shimosegawa T, Iinuma K, Ito S, Matsuno S, Abe T: Identification of thyroid hormone transporters in humans: different molecules are involved in a tissue-specific manner. Endocrinology. 2001 May;142(5):2005-12. [PubMed:11316767 ]
  2. Mikkaichi T, Suzuki T, Onogawa T, Tanemoto M, Mizutamari H, Okada M, Chaki T, Masuda S, Tokui T, Eto N, Abe M, Satoh F, Unno M, Hishinuma T, Inui K, Ito S, Goto J, Abe T: Isolation and characterization of a digoxin transporter and its rat homologue expressed in the kidney. Proc Natl Acad Sci U S A. 2004 Mar 9;101(10):3569-74. Epub 2004 Mar 1. [PubMed:14993604 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenadine. Transports benzylpenicillin (PCG), estrone-3-sulfate (E1S), cimetidine (CMD), 2,4-dichloro-phenoxyacetate (2,4-D), p-amino-hippurate (PAH), acyclovir (ACV) and ochratoxin (OTA).
Gene Name:
SLC22A8
Uniprot ID:
Q8TCC7
Molecular Weight:
59855.585 Da
References
  1. Ohtsuki S, Kikkawa T, Mori S, Hori S, Takanaga H, Otagiri M, Terasaki T: Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier. J Pharmacol Exp Ther. 2004 Jun;309(3):1273-81. Epub 2004 Feb 4. [PubMed:14762099 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Sodium-independent transporter that mediates the update of aromatic acid. Can function as a net efflux pathway for aromatic amino acids in the basosolateral epithelial cells (By similarity).
Gene Name:
SLC16A10
Uniprot ID:
Q8TF71
Molecular Weight:
55492.07 Da
References
  1. Kim DK, Kanai Y, Chairoungdua A, Matsuo H, Cha SH, Endou H: Expression cloning of a Na+-independent aromatic amino acid transporter with structural similarity to H+/monocarboxylate transporters. J Biol Chem. 2001 May 18;276(20):17221-8. Epub 2001 Feb 20. [PubMed:11278508 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Ashida K, Katsura T, Motohashi H, Saito H, Inui K: Thyroid hormone regulates the activity and expression of the peptide transporter PEPT1 in Caco-2 cells. Am J Physiol Gastrointest Liver Physiol. 2002 Apr;282(4):G617-23. [PubMed:11897620 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Peptide antigen binding
Specific Function:
Sodium-independent, high-affinity transport of large neutral amino acids such as phenylalanine, tyrosine, leucine, arginine and tryptophan, when associated with SLC3A2/4F2hc. Involved in cellular amino acid uptake. Acts as an amino acid exchanger. Involved in the transport of L-DOPA across the blood-brain barrier, and that of thyroid hormones triiodothyronine (T3) and thyroxine (T4) across the ...
Gene Name:
SLC7A5
Uniprot ID:
Q01650
Molecular Weight:
55009.62 Da
References
  1. Uchino H, Kanai Y, Kim DK, Wempe MF, Chairoungdua A, Morimoto E, Anders MW, Endou H: Transport of amino acid-related compounds mediated by L-type amino acid transporter 1 (LAT1): insights into the mechanisms of substrate recognition. Mol Pharmacol. 2002 Apr;61(4):729-37. [PubMed:11901210 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23